Art. -Nr.: HY-136351

THZ-P1-2

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC₅₀ of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.

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Reinheit: 99.86%
CAS. Nr.: 2058075-45-7
Formel: C₃₁H₂₉N₇O₂
Molecular Weight:531.61

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

THZ-P1-2 Chemical Structure

CAS. Nr.: 2058075-45-7

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

THZ-P1-2 (0.2-11.4 μM) exhibits approximately 75% inhibition of PI-4,5-P2 formation by PI5P4Kα and PI5P4Kγ and 50% inhibition by PI5P4Kβ at a concentration of 0.7 μM^[1].
THZ-P1-2 (10 nM-100 μM; 72 h) shows modest anti-proliferative activity in all six AML/ALL cell lines with IC₅₀ values in the low micromolar range^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

THP1, SEMK2, OCI/AML-2, HL60, SKM1, NOMO1 cells
Concentration:

10-100000 nM
Incubation Time:

72 hours
Result:

Showed anti-proliferative activity in all six AML/ALL cell lines with IC₅₀ values ranging from 0.87 to 3.95 μM.

Chemical Information

CAS. Nr. 2058075-45-7
Appearance Solid
Molecular Weight 531.61
Formel C₃₁H₂₉N₇O₂
Color Light yellow to yellow
SMILES

O=C(C(C=C1)=CC=C1NC(/C=C/CN(C)C)=O)NC2=CC=CC(NC3=CC(C4=CNC5=CC=CC=C45)=NC=N3)=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Journal Impact Factor

Nat Commun

PIP4K2B is mechanoresponsive and controls heterochromatin-driven nuclear softening through UHRF1. [Abstract]

2023 Mar 14;14(1):1432. PMID: 36918565

THZ-P1-2 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 14;14(1):1432. [Abstract]

THZ-P1-2 (5, 10 µM; 24 h) leads to impairment of UHRF1 levels in hTERT-RPE1 cells.
Int J Mol Sci

Pharmacological Inhibition of PIP4K2 Potentiates Venetoclax-Induced Apoptosis in Acute Myeloid Leukemia. [Abstract]

2023 Nov 29;24(23):16899. PMID: 38069220

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (188.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8811 mL

9.4054 mL

18.8108 mL

5 mM

0.3762 mL

1.8811 mL

3.7622 mL

10 mM

0.1881 mL

0.9405 mL

1.8811 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 25 mg/mL (47.03 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (250.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sivakumaren SC, et al. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 2020;27(5):525‐537.e6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8811 mL	9.4054 mL	18.8108 mL	47.0270 mL
	5 mM	0.3762 mL	1.8811 mL	3.7622 mL	9.4054 mL
	10 mM	0.1881 mL	0.9405 mL	1.8811 mL	4.7027 mL
	15 mM	0.1254 mL	0.6270 mL	1.2541 mL	3.1351 mL
	20 mM	0.0941 mL	0.4703 mL	0.9405 mL	2.3513 mL
	25 mM	0.0752 mL	0.3762 mL	0.7524 mL	1.8811 mL
	30 mM	0.0627 mL	0.3135 mL	0.6270 mL	1.5676 mL
	40 mM	0.0470 mL	0.2351 mL	0.4703 mL	1.1757 mL
	50 mM	0.0376 mL	0.1881 mL	0.3762 mL	0.9405 mL
	60 mM	0.0314 mL	0.1568 mL	0.3135 mL	0.7838 mL
	80 mM	0.0235 mL	0.1176 mL	0.2351 mL	0.5878 mL
	100 mM	0.0188 mL	0.0941 mL	0.1881 mL	0.4703 mL

Keywords

THZ-P1-2

2 Cited Publications

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THZ-P1-2

Anti-Cancer Compound Library

Autophagy Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) THZ-P1-2

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THZ-P1-2

Anti-Cancer Compound Library

Autophagy Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) THZ-P1-2

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THZ-P1-2 Related Classifications

HY-136351 Related Classifications